AG-1478 (Tyrphostin AG-1478) is a highly potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with an IC50 of 3 nM. AG-1478 (Tyrphostin AG-1478) reversibly prevents rat brain Kv1.5 potassium channels (IC50 = 9.8 mM) independent of PTK activity. Additionally, AG-1478 (Tyrphostin AG-1478) also suppresses the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 mM, respectively. AG-1478 (Tyrphostin AG-1478) blocke the activation of MAP kinase and strongly represses induction of fos gene expression and DNA synthesis. AG-1478 (Tyrphostin AG-1478) blocks G3 enhanced effects on cell apoptosis.
Aging (Albany NY). 2020 Oct 28;12(20):20801-20816.
Synergistic effect between LH and estrogen in the acceleration of cumulus expansion via GPR30 and EGFR pathways
AG-1478 purchased from AbMole
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Source | Aging (Albany NY) (2020), Figure 5, AG-1478 (AbMole Bioscience, TX, USA) |
| Method | western blot | |
| Cell Lines | cumulus cells | |
| Concentrations | 3 μM | |
| Incubation Time | 8 h | |
| Results | The mRNA of GPR30 was downregulated by EGF stimulation, while AG1478 reversed the inhibition of GPR30 transcription caused by EGF treatment |
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Source | Aging (Albany NY) (2020), Figure 4, AG-1478 (AbMole Bioscience, TX, USA) |
| Method | intraperitoneal injection | |
| Cell Lines | mice | |
| Concentrations | 1 mg/kg body weight | |
| Incubation Time | 1, 3, 5, and 7 day | |
| Results | The results showed that hCG significantly activated p-EGFR (Tyr1068), but AG1478 blocked the activation of p-EGFR induced by hCG stimulation |
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Source | Sci Rep (2018). Figure 4. AG-1478 |
| Method | western blotting | |
| Cell Lines | corneal endothelial cells | |
| Concentrations | 1 μM | |
| Incubation Time | 7 days | |
| Results | The addition of TGF-β1 (with or without AG-1478) also generated the expression of n-cadherin at the cell membrane. The gain of n-cadherin expression following addition of TGF-β1 was confirmed using western blotting |
| Molecular Weight | 315.75 |
| Formula | C16H14ClN3O2 |
| CAS Number | 153436-53-4 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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